Molecular Insights to the Structure-Interaction Relationships of Human Proton-Coupled Oligopeptide Transporters (PepTs).
Molecular Insights to the Structure-Interaction Relationships of Human Proton-Coupled Oligopeptide Transporters (PepTs).
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DOI：
10.3390/pharmaceutics15102517
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发表时间：
2023-10-23
期刊：
影响因子：
5.4
通讯作者：
Zhou F
中科院分区：
文献类型：
--
作者：
Luo Y;Gao J;Jiang X;Zhu L;Zhou QT;Murray M;Li J;Zhou F
人质子偶联寡肽转运蛋白（PepTs）是重要的膜内流转运蛋白，促进包括ACE抑制剂和抗生素在内的许多药物的细胞摄取。多肽介导膳食蛋白质或胃肠道分泌物对二肽和三肽的吸收，促进肾脏中多肽结合氨基酸的重吸收，并调节细胞外液中神经肽的稳态。在所有PepT亚型中，对PepT1和PepT2的研究最为深入。调节PepTs及其药物底物的相互作用可能影响某些疗法的治疗结果和不良反应。近年来，研究人员建立了PepTs的拓扑模型和蛋白质结构。这篇综述的目的是总结目前关于PepTs及其底物的结构-相互作用关系（SIRs）的知识，以及这些信息在治疗优化和药物开发中的潜在应用。这些信息可能有助于深入了解PepT药物底物对患者的疗效、药物-药物/食物相互作用的机制以及PepT靶向在药物设计和开发策略中的潜在作用。
Human proton-coupled oligopeptide transporters (PepTs) are important membrane influx transporters that facilitate the cellular uptake of many drugs including ACE inhibitors and antibiotics. PepTs mediate the absorption of di- and tri-peptides from dietary proteins or gastrointestinal secretions, facilitate the reabsorption of peptide-bound amino acids in the kidney, and regulate neuropeptide homeostasis in extracellular fluids. PepT1 and PepT2 have been the most intensively investigated of all PepT isoforms. Modulating the interactions of PepTs and their drug substrates could influence treatment outcomes and adverse effects with certain therapies. In recent studies, topology models and protein structures of PepTs have been developed. The aim of this review was to summarise the current knowledge regarding structure-interaction relationships (SIRs) of PepTs and their substrates as well as the potential applications of this information in therapeutic optimisation and drug development. Such information may provide insights into the efficacy of PepT drug substrates in patients, mechanisms of drug–drug/food interactions and the potential role of PepTs targeting in drug design and development strategies.
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